EP3946293A4 - COMPOUNDS WITH ANTITUMOR ACTIVITY AGAINST CANCER CELLS CARRYING EGFR OR HER2 EXON 20 INSERTS - Google Patents

COMPOUNDS WITH ANTITUMOR ACTIVITY AGAINST CANCER CELLS CARRYING EGFR OR HER2 EXON 20 INSERTS Download PDF

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Publication number
EP3946293A4
EP3946293A4 EP20783802.0A EP20783802A EP3946293A4 EP 3946293 A4 EP3946293 A4 EP 3946293A4 EP 20783802 A EP20783802 A EP 20783802A EP 3946293 A4 EP3946293 A4 EP 3946293A4
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EP
European Patent Office
Prior art keywords
inserts
compounds
cancer cells
activity against
antitumor activity
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Pending
Application number
EP20783802.0A
Other languages
German (de)
French (fr)
Other versions
EP3946293A1 (en
Inventor
John V. HEYMACH
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
University of Texas System
University of Texas at Austin
Original Assignee
University of Texas System
University of Texas at Austin
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Publication date
Application filed by University of Texas System, University of Texas at Austin filed Critical University of Texas System
Publication of EP3946293A1 publication Critical patent/EP3946293A1/en
Publication of EP3946293A4 publication Critical patent/EP3946293A4/en
Pending legal-status Critical Current

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/436—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/66—Phosphorus compounds
    • A61K31/675—Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/705—Receptors; Cell surface antigens; Cell surface determinants
    • C07K14/71—Receptors; Cell surface antigens; Cell surface determinants for growth factors; for growth regulators
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12Q—MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
    • C12Q1/00—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions
    • C12Q1/68—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving nucleic acids
    • C12Q1/6876—Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes
    • C12Q1/6883—Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes for diseases caused by alterations of genetic material
    • C12Q1/6886—Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes for diseases caused by alterations of genetic material for cancer
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12Q—MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
    • C12Q2600/00—Oligonucleotides characterized by their use
    • C12Q2600/106—Pharmacogenomics, i.e. genetic variability in individual responses to drugs and drug metabolism
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12Q—MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
    • C12Q2600/00—Oligonucleotides characterized by their use
    • C12Q2600/156—Polymorphic or mutational markers

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  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Genetics & Genomics (AREA)
  • Zoology (AREA)
  • Immunology (AREA)
  • Analytical Chemistry (AREA)
  • Pathology (AREA)
  • Wood Science & Technology (AREA)
  • Engineering & Computer Science (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Physics & Mathematics (AREA)
  • General Engineering & Computer Science (AREA)
  • Hospice & Palliative Care (AREA)
  • Microbiology (AREA)
  • Biotechnology (AREA)
  • Oncology (AREA)
  • Cell Biology (AREA)
  • Toxicology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (AREA)
EP20783802.0A 2019-03-29 2020-03-27 COMPOUNDS WITH ANTITUMOR ACTIVITY AGAINST CANCER CELLS CARRYING EGFR OR HER2 EXON 20 INSERTS Pending EP3946293A4 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201962826843P 2019-03-29 2019-03-29
PCT/US2020/025228 WO2020205521A1 (en) 2019-03-29 2020-03-27 Compounds with anti-tumor activity against cancer cells bearing egfr or her2 exon 20 insertions

Publications (2)

Publication Number Publication Date
EP3946293A1 EP3946293A1 (en) 2022-02-09
EP3946293A4 true EP3946293A4 (en) 2023-05-03

Family

ID=72666976

Family Applications (1)

Application Number Title Priority Date Filing Date
EP20783802.0A Pending EP3946293A4 (en) 2019-03-29 2020-03-27 COMPOUNDS WITH ANTITUMOR ACTIVITY AGAINST CANCER CELLS CARRYING EGFR OR HER2 EXON 20 INSERTS

Country Status (13)

Country Link
US (2) US20220143023A1 (en)
EP (1) EP3946293A4 (en)
JP (2) JP7650814B2 (en)
KR (1) KR20210149103A (en)
CN (1) CN113939284A (en)
AU (1) AU2020254499A1 (en)
BR (1) BR112021019489A2 (en)
CA (1) CA3131864A1 (en)
IL (1) IL286742A (en)
MX (1) MX2021011948A (en)
PH (1) PH12021552395A1 (en)
SG (1) SG11202110669WA (en)
WO (1) WO2020205521A1 (en)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN110129434A (en) * 2018-02-08 2019-08-16 埃提斯生物技术（上海）有限公司 Application of the biomarker in diagnosing malignant tumor in bile
BR112021016149A2 (en) 2019-02-26 2021-10-13 Janssen Biotech, Inc. COMBINATION THERAPIES AND STRATIFICATION OF PATIENTS WITH B-SPECIFIC ANTI-EGFR/C-MET ANTIBODIES
MX2021011948A (en) * 2019-03-29 2022-01-04 Univ Texas Compounds with anti-tumor activity against cancer cells bearing egfr or her2 exon 20 insertions.
EP3956035A4 (en) * 2019-04-17 2023-01-25 Board of Regents, The University of Texas System CANCER COMPOUNDS CARRYING EGFR MUTATIONS RESISTANT TO TYROSINE KINASE INHIBITORS
US11850248B2 (en) 2019-05-14 2023-12-26 Yuhan Corporation Therapies with 3rd generation EGFR tyrosine kinase inhibitors
US11879013B2 (en) 2019-05-14 2024-01-23 Janssen Biotech, Inc. Combination therapies with bispecific anti-EGFR/c-Met antibodies and third generation EGFR tyrosine kinase inhibitors
JP7783182B2 (en) 2020-02-12 2025-12-09 ヤンセン バイオテツク，インコーポレーテツド Treatment of patients with c-MET exon 14 skipping mutations
PY21113397A (en) * 2020-12-29 2022-10-12 Spectrum Pharmaceuticals Inc TREATMENT FOR MALIGNANT SOLID TUMORS
WO2022206929A1 (en) * 2021-04-01 2022-10-06 上海医药集团股份有限公司 Application of compound in preparation of inhibitory drug targeting erbb2 mutant
WO2023015149A1 (en) * 2021-08-02 2023-02-09 Spectrum Pharmaceuticals, Inc. Treatment of non-small cell lung cancer with poziotinib
KR20230063731A (en) 2021-11-02 2023-05-09 주식회사 엘지에너지솔루션 Manufacturing method of secondary battery using split injections of electrolyte

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2018094225A1 (en) * 2016-11-17 2018-05-24 Board Of Regents, The University Of Texas System Compounds with anti-tumor activity against cancer cells bearing egfr or her2 exon 20 mutations
EP3773551A2 (en) * 2018-03-27 2021-02-17 Board of Regents, The University of Texas System Compounds with anti-tumor activity against cancer cells bearing her2 exon 19 mutations

Family Cites Families (4)

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US10308658B2 (en) * 2015-10-19 2019-06-04 Sunshine Lake Pharma Co., Ltd. Salt of EGFR inhibitor, crystalline form and uses thereof
EP3687542A1 (en) * 2017-09-27 2020-08-05 AI Therapeutics, Inc. Therapeutic methods relating to hsp90 inhibitors
WO2019178239A1 (en) * 2018-03-13 2019-09-19 Board Of Regents, The University Of Texas System Methods for treatment of cancers with egfr activating mutations
MX2021011948A (en) * 2019-03-29 2022-01-04 Univ Texas Compounds with anti-tumor activity against cancer cells bearing egfr or her2 exon 20 insertions.

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2018094225A1 (en) * 2016-11-17 2018-05-24 Board Of Regents, The University Of Texas System Compounds with anti-tumor activity against cancer cells bearing egfr or her2 exon 20 mutations
EP3773551A2 (en) * 2018-03-27 2021-02-17 Board of Regents, The University of Texas System Compounds with anti-tumor activity against cancer cells bearing her2 exon 19 mutations

Non-Patent Citations (10)

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Title
ANONYMOUS: "A Phase 1 b Study of Poziotinib in Combination With T-DM1 in Women With Advanced or Metastatic HER2-Positive Breast Cancer", CLINICAL STUDY RECORD, 8 February 2018 (2018-02-08), pages 1 - 4, XP055721106, Retrieved from the Internet <URL:https://clinicaltrials.gov/ct2/history/NCT03429101?A=1&B=1&C=merged#StudyPageTop> [retrieved on 20200810] *
CARDONA ANDR�S F ET AL: "EGFR exon 20 insertion in lung adenocarcinomas among Hispanics (geno1.2-CLICaP)", LUNG CANCER, ELSEVIER, AMSTERDAM, NL, vol. 125, 9 October 2018 (2018-10-09), pages 265 - 272, XP085524047, ISSN: 0169-5002, DOI: 10.1016/J.LUNGCAN.2018.10.007 *
KEN SUZAWA ET AL: "Antitumor effect of afatinib, as a human epidermal growth factor receptor 2-targeted therapy, in lung cancers harboring HER2 oncogene alterations", CANCER SCIENCE, vol. 107, no. 1, 3 December 2015 (2015-12-03), JP, pages 45 - 52, XP055486111, ISSN: 1347-9032, DOI: 10.1111/cas.12845 *
MEHTA RUTIKA: "The Role of HER2 Testing in Advanced Colorectal Cancer", CURRENT COLORECTAL CANCER REPORTS, SPRINGER US, BOSTON, vol. 14, no. 6, 29 October 2018 (2018-10-29), pages 184 - 191, XP037917947, ISSN: 1556-3790, [retrieved on 20181029], DOI: 10.1007/S11888-018-0417-6 *
R. BOSE ET AL: "Activating HER2 Mutations in HER2 Gene Amplification Negative Breast Cancer", CANCER DISCOVERY, vol. 3, no. 2, 1 February 2013 (2013-02-01), US, pages 224 - 237, XP055308237, ISSN: 2159-8274, DOI: 10.1158/2159-8290.CD-12-0349 *
See also references of WO2020205521A1 *
SHE-JUAN AN ET AL: "Identification of Enriched Driver Gene Alterations in Subgroups of Non-Small Cell Lung Cancer Patients Based on Histology and Smoking Status", PLOS ONE, vol. 7, no. 6, 29 June 2012 (2012-06-29), pages e40109, XP055420056, DOI: 10.1371/journal.pone.0040109 *
WENHSIANG WEN ET AL: "Mutations in the Kinase Domain of the HER2/ERBB2 Gene Identified in a Wide Variety of Human Cancers", THE JOURNAL OF MOLECULAR DIAGNOSTICS, vol. 17, no. 5, 30 September 2015 (2015-09-30), pages 487 - 495, XP055744635, ISSN: 1525-1578, DOI: 10.1016/j.jmoldx.2015.04.003 *
WOO HYUN SUN ET AL: "Epidermal growth factor receptor (EGFR) exon 20 mutations in non-small-cell lung cancer and resistance to EGFR-tyrosine kinase inhibitors", INVESTIGATIONAL NEW DRUGS, SPRINGER US, NEW YORK, vol. 32, no. 6, 23 August 2014 (2014-08-23), pages 1311 - 1315, XP035702639, ISSN: 0167-6997, [retrieved on 20140823], DOI: 10.1007/S10637-014-0146-X *
YANG CHING-YAO ET AL: "Programmed cell death-ligand 1 expression is associated with a favourable immune microenvironment and better overall survival in stage I pulmonary squamous cell carcinoma", EUROPEAN JOURNAL OF CANCER, ELSEVIER, AMSTERDAM NL, vol. 57, 21 February 2016 (2016-02-21), pages 91 - 103, XP029445049, ISSN: 0959-8049, DOI: 10.1016/J.EJCA.2015.12.033 *

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Publication number Publication date
JP2022527788A (en) 2022-06-06
JP7650814B2 (en) 2025-03-25
US20220143023A1 (en) 2022-05-12
US20250312348A1 (en) 2025-10-09
MX2021011948A (en) 2022-01-04
EP3946293A1 (en) 2022-02-09
KR20210149103A (en) 2021-12-08
SG11202110669WA (en) 2021-10-28
CN113939284A (en) 2022-01-14
JP2025090740A (en) 2025-06-17
BR112021019489A2 (en) 2022-02-08
CA3131864A1 (en) 2020-10-08
IL286742A (en) 2021-10-31
WO2020205521A1 (en) 2020-10-08
PH12021552395A1 (en) 2022-06-13
AU2020254499A1 (en) 2021-10-28

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